Metoprolol
(Synonyms: 美托洛尔) 目录号 : GC36603
Metoprolol是一种选择性β1受体阻滞剂。
Cas No.:51384-51-1
Sample solution is provided at 25 µL, 10mM.
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Metoprolol is a selective β1 receptor blocker [1]. Metoprolol slows down the heart rate, reduces myocardial contractility and cardiac output by inhibiting β1-adrenergic receptors in the heart, thereby reducing myocardial oxygen consumption and stabilizing heart rhythm [2]. Metoprolol is commonly used to treat hypertension, angina pectoris, arrhythmia and other diseases [3-4].
In human retinal endothelial cells (HREC), Metoprolol (1µM, 10µM; 24h, 48h) counteracts the increase in the tube-like structures of HREC stimulated with high glucose [5]. In rat cardiac myocytes, Metoprolol (3µM; 12h) but not carvedilol prevents isoprenaline-induced downregulation of myocyte b-adrenoceptors [6]. In neutrophils, Metoprolol (0.3-300µM; 40min) dose-dependently inhibits neutrophil migration induced by formyl peptide [7].
In isoflurane anesthetized mice models, Metoprolol (3mg/kg; iv; single injection) caused a reduction in HR, SV, and CO, while SVR increased [8]. In ApoE-/- mice, Metoprolol (2.5mg/kg; iv; 11 weeks) reduced atherosclerotic plaque area [9]. In collagenase-injection intracerebral hemorrhage (ICH) mice model Metoprolol (2.5mg/kg; ig; 14d) attenuates intracerebral hemorrhage-induced cardiac damage by suppression of sympathetic overactivity [10].
References:
[1]. Koch-Weser J. Metoprolol. New England Journal of Medicine. 1979 Sep 27; 301(13): 698-703.
[2]. Rangno RE, Langlois S, Lutterodt A. Metoprolol withdrawal phenomena: mechanism and prevention. Clinical Pharmacology & Therapeutics. 1982 Jan; 31(1): 8-15.
[3]. Merit-HF Study Group. Effect of metoprolol CR/XL in chronic heart failure: metoprolol CR/XL randomised intervention trial in-congestive heart failure (MERIT-HF). The Lancet. 1999 Jun 12;353(9169): 2001-2007.
[4]. Brogden RN, Heel RC, Speight TM, et al. Metoprolol: a review of its pharmacological properties and therapeutic efficacy in hypertension and angina pectoris. Drugs. 1977 Nov; 14: 321-348.
[5]. Giurdanella G, Longo A, Distefano A, et al. The anti-inflammatory effect of the β1-adrenergic receptor antagonist metoprolol on high glucose treated human microvascular retinal endothelial cells. Cells. 2021 Dec 24; 11(1): 51.
[6]. Flesch M, Ettelbrück S, Rosenkranz S, Maack C, Cremers B, Schlüter KD, Zolk O, Böhm M. Differential effects of carvedilol and metoprolol on isoprenaline-induced changes in β-adrenoceptor density and systolic function in rat cardiac myocytes. Cardiovascular research. 2001 Feb 1; 49(2): 371-380.
[7]. Dunzendorfer S, Wiedermann CJ. Modulation of neutrophil migration and superoxide anion release by metoprolol. Journal of molecular and cellular cardiology. 2000 Jun 1; 32(6): 915-924.
[8]. El Beheiry MH, Heximer SP, Voigtlaender-Bolz J, et al. Metoprolol impairs resistance artery function in mice. Journal of Applied Physiology. 2011 Oct; 111(4): 1125-1133.
[9]. Ulleryd MA, Bernberg E, Yang LJ, et al. Metoprolol reduces proinflammatory cytokines and atherosclerosis in ApoE−/− mice. BioMed research international. 2014; 2014(1): 548783.
[10]. Zhang L, Wuri J, An L, et al. Metoprolol attenuates intracerebral hemorrhage-induced cardiac damage by suppression of sympathetic overactivity in mice. Autonomic Neuroscience. 2021 Sep 1; 234: 102832.
Metoprolol是一种选择性β1受体阻滞剂 [1]。Metoprolol通过抑制心脏内的β1-肾上腺素受体，减慢心率，降低心肌收缩力和心输出量，从而降低心肌耗氧量，稳定心律 [2]。Metoprolol常用于治疗高血压、心绞痛、心律失常等疾病 [3-4]。
在人视网膜内皮细胞（HREC）中，Metoprolol（1µM、10µM；24h、48h）可抵消高葡萄糖刺激后HREC管状结构的增加 [5]。在大鼠心肌细胞中，Metoprolol（3µM；12h）能阻止异丙肾上腺素诱导的心肌细胞β-肾上腺素能受体下调，而卡维地洛则不能 [6]. 在中性粒细胞中，Metoprolol（0.3-300µM；40分钟）剂量依赖性地抑制甲酰肽诱导的中性粒细胞迁移 [7]。
在异氟烷麻醉小鼠模型中，Metoprolol（3mg/kg；iv；单次注射）导致HR、SV和CO降低，而SVR增加 [8]。在 ApoE-/-小鼠中，Metoprolol（2.5mg/kg；iv；11周）减少了动脉粥样硬化斑块面积 [9]。在胶原酶注射脑出血（ICH）小鼠模型中，Metoprolol（2.5mg/kg；ig；14d）通过抑制交感神经过度活跃来减轻脑出血引起的心脏损害 [10]。
| Cell experiment [1]: | |
Cell lines | Human retinal endothelial cells (HREC) |
Preparation Method | Before HREC seeding, the flasks or dishes were pre-coated with a bovine plasma fibronectin at a concentration of 1 mg/mL (Innoprot) for 1h at 37℃ in a humidified atmosphere of 5% CO2 and were subsequently rinsed twice with sterile water. Before the treatments, HREC were incubated with medium containing 2.5% FBS that was supplemented ECM for 4h before treatments. The cells were then treated with 5mM glucose (normal glucose or NG, control condition) or with 25mM glucose (high glucose, HG) in 2.5% FBS ECM medium for 24-48h in the absence or in the presence of 1 and 10μM of Metoprolol and/or 1 and 10μM of epinephrine. The cells were treated after reaching about 70% confluence and were used at passages 3 and 9. After treatment, the cells were washed twice in PBS and subjected to subsequent analyses. |
Reaction Conditions | 1µM, 10µM; 24h, 48h |
Applications | Metoprolol counteracts the increase in the tube-like structures of HREC stimulated with high glucose. |
| Animal experiment [2]: | |
Animal models | Isoflurane anesthetized mice models |
Preparation Method | In a group of anesthetized C57BL6/J mice, femoral artery and vein cannulations were performed to measure mean arterial pressure (MAP) and heart rate (HR) following administration of saline vehicle or Metoprolol (3mg/kg). |
Dosage form | 3mg/kg; iv; single injection |
Applications | In isoflurane anesthetized mice, Metoprolol caused a reduction in HR, SV, and CO, while SVR increased. |
References: | |
| Cas No. | 51384-51-1 | SDF | |
| 别名 | 美托洛尔 | ||
| Canonical SMILES | OC(CNC(C)C)COC1=CC=C(CCOC)C=C1 | ||
| 分子式 | C15H25NO3 | 分子量 | 267.36 |
| 溶解度 | DMSO : 53mg/mL | 储存条件 | Store at -20°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7403 mL | 18.7014 mL | 37.4028 mL |
| 5 mM | 0.7481 mL | 3.7403 mL | 7.4806 mL |
| 10 mM | 0.374 mL | 1.8701 mL | 3.7403 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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